This study is a single-center, open-label, single-dose trial performed in a randomized, four-way, change-over design in healthy volunteers. The primary purpose of this study is to evaluate the effect of moderate heat, occlusion, and moderate exercise on pharmacokinetics. The secondary purpose is to characterize the effect of special conditions on the bioavailability and to evaluate patch adhesion and safety of TK-254RX and a residual amount of the patch.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
28
TK-254RX will be applied for one day
SocraTec R&D GmbH Clinical Pharmacology Unit
Mainzerhofplatz, Erfurt, Germany
Assessing the effect of each intervention by Area under the plasma concentration versus time curve over 24 hours (AUC0-24) of S-flurbiprofen
assessment of the effect of heat, occlusion, and moderate exercise on Test by use of AUC0-24 of S flurbiprofen
Time frame: Day 1 to Day 2 for each period
Assessing the effect of each intervention by peak plasma concentration (Cmax) of S-flurbiprofen
assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of Cmax of S flurbiprofen
Time frame: Day 1 to Day 2 for each period
Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to last measurement time point with a concentration value above lower limit of quantitation (AUC0-tlast) of S-flurbiprofen
assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of AUC0-tlast of S flurbiprofen
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to infinity (AUC0-inf) of S-flurbiprofen
assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of AUC0-inf of S flurbiprofen
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by area under the curve over 24 hours (AUC0-24)
Characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by AUC0-24 of R-flurbiprofen and metabolites, if applicable
Time frame: Day 1 to Day 2 for each period
Assessing the effect of each intervention by peak plasma concentration (Cmax)
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Characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Cmax of R-flurbiprofen and metabolites, if applicable
Time frame: Day 1 to Day 2 for each period
Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to last time point with a concentration value above lower limit of quantitation (AUC0-tlast)
Characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by AUC0-tlast of R-flurbiprofen and metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by area under plasma concentration versus time curve from patch application to infinity (AUC0-inf)
Characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by AUC0-inf of R-flurbiprofen and metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by percentage of area under the plasma concentration versus time curve extrapolated to infinity to area under the plasma concentration versus time curve from 0 hour to infinity (AUCexpol%)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by AUCexpol% of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by concentration at the last time point with concentration value above lower limit of quantitation (Clast)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Clast of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 2 for each period
Assessing the effect of each intervention by time point to reach peak plasma concentration (Tmax)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Tmax of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Asssessing the effect of each intervention by last time point with concentration value above the lower limit of quantitation (Tlast)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Tlast of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by apparent terminal elimination half-life (T1/2)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by T1/2 of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by apparent terminal elimination rate constant determined by log-linear regression (Lz)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Lz of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 4 for each period
Assessing the effect of each intervention by time point before first concentration balue above the lower limit quantitation (Tlag)
characterisation of the effect of heat, occlusion, and moderate exercise on the bioavailability of Test determined by Tlag of S flurbiprofen as well as R flurbiprofen and their metabolites, if applicable
Time frame: Day 1 to Day 2 for each period
Characterization of EFTS adhesion
measuring patch adhesion area by percentage of visually by site staff with remaining patch adhered
Time frame: Day 2 for each period
Characterization of local tolerability
Assessing the local tolerability by using the 8-point dermal response and other effects score according to FDA recommendation
Time frame: with in 5 minutes after removal of each patch as well as 12 hours, 24 hours, and 36 hours after removal for each period
Recording adverse event and serious adverse event
Time frame: Day 1 to Day 4 for each period
Residual amount
residual amout of S-flurbiprofen in used patch for each period
Time frame: Day 2 for each period